Indacaterol - CAS 312753-06-3
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Adrenergic Receptor
Indacaterol Maleate is an ultra-long-acting β-adrenoceptor agonist.
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Arcapta maleate; Onbrez maleate
1.Safety Considerations with Dual Bronchodilator Therapy in COPD: An Update.
Matera MG1, Rogliani P2, Calzetta L2, Cazzola M3. Drug Saf. 2016 Feb 29. [Epub ahead of print]
Combining a long-acting β2-agonist (LABA) with a long-acting anti-muscarinic agent (LAMA) provides synergistic benefit on airway smooth muscle relaxation, which may have major implications for the use of LABA/LAMA combinations in the treatment of chronic obstructive pulmonary disease (COPD). There are four different approved LAMA/LABA fixed-dose combinations (FDCs)-glycopyrronium/indacaterol, umeclidinium/vilanterol, tiotropium/olodaterol, and aclidinium/formoterol-and another, glycopyrronium/formoterol, that is still under clinical development. Many pivotal trials have shown that all of these FDCs are more effective than monotherapies in inducing bronchodilation and do not amplify the possible adverse events (AEs) that are characteristic of LAMAs and LABAs when used as monotherapy. Unfortunately, these clinical trials have included a very small and highly selected fraction of the COPD patient population. Therefore, it is questionable whether such data can be extrapolated to a larger, 'real-life' population of patients with COPD, especially given that COPD patients with co-morbidities are often excluded from clinical trials, COPD is a major risk factor for most cardiovascular diseases, and both LAMAs and LABAs have a high potential to impact cardiac activities.
2.Population pharmacokinetics of IND/GLY (indacaterol/glycopyrronium) in COPD patients.
Demin I, Bartels C, Graham G, Bieth B, Gautier A, Tillmann HC, Sechaud R. Int J Clin Pharmacol Ther. 2016 Apr 6. [Epub ahead of print]
OBJECTIVE: Indacaterol/glycopyrronium (IND/GLY) is a fixed-dose combination (FDC) of indacaterol, an inhaled long-acting β2-agonist (LABA), and glycopyrronium, an inhaled long-acting muscarinic antagonist (LAMA), developed as a maintenance bronchodilator treatment for patients with chronic obstructive pulmonary disease (COPD). A population pharmacokinetic (PK) analysis was performed to describe the PK profiles of indacaterol and glycopyrronium following the twice daily (b.i.d.) and once daily (o.d.) inhalation regimens as FDC or as monotherapies and to determine the effect of covariates.
3.Cost-effectiveness of umeclidinium/vilanterol combination therapy compared to tiotropium monotherapy among symptomatic patients with chronic obstructive pulmonary disease in the UK.
Punekar YS1, Roberts G2, Ismaila A3, O'Leary M2. Cost Eff Resour Alloc. 2015 Dec 12;13:22. doi: 10.1186/s12962-015-0048-6. eCollection 2015.
BACKGROUND: The cost-effectiveness of umeclidinium bromide-vilanterol (UMEC/VI) versus tiotropium monotherapy in the UK was assessed using a UMEC/VI treatment-specific economic model based on a chronic obstructive pulmonary disease (COPD) disease-progression model.
4.Differential pharmacology and clinical utility of long-acting bronchodilators in COPD - focus on olodaterol.
Matera MG1, Ora J2, Cazzola M3. Ther Clin Risk Manag. 2015 Dec 4;11:1805-11. doi: 10.2147/TCRM.S73581. eCollection 2015.
Olodaterol (BI 1744 CL) is a novel, once-daily long-acting β2-agonist (LABA) designed with the aim of improving β2-adrenoreceptor selectivity and intrinsic activity. Phase III pivotal trials have documented that olodaterol Respimat Soft Mist inhaler 5 μg induces fast onset of bronchodilation, comparable with formoterol at day 1. Moreover, significant lung function improvements have been documented up to 48 weeks in patients with moderate to very severe chronic obstructive pulmonary disease (COPD). Olodaterol was generally well tolerated and had an acceptable cardiovascular and respiratory adverse event profile. Regrettably, the clinical development of olodaterol is however still too partial to draw any firm conclusions on the positioning of this ultra-LABA as monotherapy in the management of COPD. Waiting for further data on the impact of olodaterol on different patient-reported outcomes, which however are widely available for indacaterol, and mainly for a head-to-head comparison between these two ultra-LABAs and between olodaterol long-acting antimuscarinic antagonists other than tiotropium, we believe it is correct to follow the clinical indications of indacaterol also for olodaterol.
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CAS 312753-06-3 Indacaterol

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